Salicylidene salicylhydrazide, a selective inhibitor of β1-containing GABA A receptors

British Journal of Pharmacology

Volumn 142, Issue 1, 2004, Pages 97-106

  Thompson, S A ^a   Wheat, L ^a,b   Brown, N A ^a   Wingrove, P B ^a   Pillai, G V ^a   Whiting, P J ^a   Adkins, C ^a   Woodward, C H ^a   Smith, A J ^a   Simpson, P B ^a   Collins, I ^a   Wafford, K A ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^b UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

subunit; Allosteric; GABA A receptor; Ion channel; Modulator; Mutagenesis; Salicylidene salicylhydrazide; Transmembrane domain

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; BICUCULLINE; FLUMAZENIL; ISOLEUCINE; LORECLEZOLE; MEFENAMIC ACID; PENTOBARBITAL; PICROTOXIN; PRASTERONE SULFATE; PREGNENOLONE; PREGNENOLONE SULFATE; RECEPTOR SUBUNIT; SALICYLIDENE SALICYLHYDRAZIDE; THREONINE; UNCLASSIFIED DRUG;

ALLOSTERISM; AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; BETA CHAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG MECHANISM; DRUG SELECTIVITY; ELECTROPHYSIOLOGY; EVALUATION; HIGH THROUGHPUT SCREENING; IC 50; INHIBITION KINETICS; MOUSE; NONHUMAN; PATCH CLAMP; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN STRUCTURE; SEQUENCE ANALYSIS;

AMINO ACID SEQUENCE; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GABA ANTAGONISTS; GAMMA-AMINOBUTYRIC ACID; HUMANS; HYDRAZINES; MOLECULAR SEQUENCE DATA; PROTEIN SUBUNITS; RECEPTORS, GABA-A; XENOPUS;

EID: 2542547342     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705689     Document Type: Article

References (29)

1. A receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J. Biol. Chem., 276, 38934-38939.
2. AINSCOUGH, E.W., BRODIE, A.M., DENNY, W.A., FINLAY, G.J., GOTHE, S.A. & RANFORD, J.D. (1999). Cytotoxicity of salicylaldehyde benzoylhydrazone analogs and their transition metal complexes: quantitative structure-activity relationships. J. Inorg. Biochem., 77, 125-133.
3. BARISH, M.E. (1983). A transient calcium-dependent chloride current in the immature Xenopus oocyte. J. Physiol. (Lond)., 342, 309-325.
4. BELELLI, D., LAMBERT, J.J., PETERS, J.A., WAFFORD, K. & WHITING, P.J. (1997). The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc. Natl. Acad. Sci. U.S.A., 94, 11031-11036.
5. A receptor M2-M3 loop secondary structure and changes in accessibility during channel gating. J. Biol. Chem., 277, 43002-43010.
6. BLANTON, M.P. & COHEN, J.B. (1994). Identifying the lipid-protein interface of the Torpedo nicotinic aeetylcholine receptor: secondary structure implications. Biochemistry, 33, 2859-2872.
7. A receptors. Br. J. Pharmacol., 136, 965-974.
8. A receptor. J. Neurosci., 16, 5415-5424.
9. FARRAR, S.J., WHITING, P.J., BONNERT, T.P. & MCKERNAN, R.M. (1999). Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer. J. Biol. Chem., 274, 10100-10104.
10. A receptors. Mol. Pharmacol., 43, 970-975.
11. HADINGHAM, K.L., WINGROVE, P.B., WAFFORD, K.A., BAIN, C., KEMP, J.A., PALMER, K.J., WILSON, A.W., WILCOX, A.S., SIKELA, J.M., RAGAN, C.I. & WHITING, P.J. (1993b). Role of the β subunit in determining the pharmacology of human γ-aminobutyric acid type A receptors. Mol. Pharmacol., 44, 1211-1218.
12. A receptors by the non-steroid anti-inflammatory agent, mefenamic acid. Eur. J. Neurosci., 11, 2897-2905.
13. HILL-VENNING, C., BELELLI, D., PETERS, J.A. & LAMBERT, J.J. (1997). Subunit-dependent interaction of the general anaesthetic etomidate with the γ-aminobutyric acid type A receptor. Br. J. Pharmacol., 120, 749-756.
14. KORPI, E.R., GRUNDER, G. & LÜDDENS, H. (2002). Drug interactions at GABA(A) receptors. Prog. Neurobiol., 67, 113-159.
15. JURD, R., ARRAS, M., LAMBERT, S., DREXLER, B., SIEGWART, R., CRESTANI, F., ZAUGG, M., VOGT, K.E., LEDERMANN, B., ANTKOWIAK, B. & RUDOLPH, U. (2003). General anesthetic actions in vivo strongly attenuated by a point mutation in the GABAA receptor β3 subunit. FASEB J., 17, 250-252.
16. A receptors: immunocytochemical distribution of 13 subunits in the adult rat brain. Neuroscience, 101, 815-850.
17. PISTIS, M., BELELLI, D., MCGURK, K., PETERS, J.A. & LAMBERT, J.J. (1999). Complementary regulation of anaesthetic activation of human (α6β3γ2L) and Drosophila (RDL) GABA receptors by a single amino acid residue. J. Physiol., 515, 3-18.
18. A receptor isoforms. J. Neurosci., 23, 8608-8617.
19. A receptor subtypes. Curr. Top. Med. Chem., 2, 795-816.
20. A receptor pharmacology and functional responses. Anal. Bioanal. Chem., 377, 843-851.
21. THOMPSON, S.A., ARDEN, S.A., MARSHALL, G., WINGROVE, P.B., WHITING, P.J. & WAFFORD, K.A. (1999). Residues in transmembrane domains I and II determine γ-aminobutyric acid type A receptor subtype-selective antagonism by furosemide. Mol. Pharmacol., 55, 993-999.
22. A receptor: dependence on receptor subunit combination. Br. J. Pharmacol., 117, 521-527.
23. THOMPSON, S.A., WINGROVE, P.B., CONNELLY, L., WHITING, P.J. & WAFFORD, K.A. (2002). Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. Mol. Pharmacol., 61, 861-869.
24. A receptor β subunit. Neuron, 12, 775-782.
25. A receptor expressed in Xenopus oocytes. Receptors Channels, 3, 1-5.
26. WHITING, P.J. (2003). GABA-A receptor subtypes in the brain: a paradigm for CNS drug discovery? Drug Discov. Today, 8, 445-450.
27. WHITING, P.J., WAFFORD, K.A., PRIBILLA, I. & PETRI, T. (1995). Channel cloning, mutagenesis, and expression. In: Ion Channels. A Practical Approach, ed. Ashley, R.H. pp. 133-169. McLean, VA: IRL Press.
28. 2+ complexation. Neuropharmacology, 43, 938-944.
29. WINGROVE, P.B., WAFFORD, K.A., BAIN, C. & WHITING, P.J. (1994). The modulatory action of loreclezole at the γ-aminobutyric acid type A receptor is determined by a single amino acid in the β2 and β3 subunit. Proc. Natl. Acad. Sci. U.S.A., 91, 4569-4573.